Search Results - "Wilks, Andrew F"

Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death by Hildebrand, Joanne M., Tanzer, Maria C., Lucet, Isabelle S., Young, Samuel N., Spall, Sukhdeep K., Sharma, Pooja, Pierotti, Catia, Garnier, Jean-Marc, Dobson, Renwick C.J., Webb, Andrew I., Tripaydonis, Anne, Babon, Jeffrey J., Mulcair, Mark D., Scanlon, Martin J., Alexander, Warren S., Wilks, Andrew F., Czabotar, Peter E., Lessene, Guillaume, Murphy, James M., Silke, John

“…Significance The four-helix bundle (4HB) domain of Mixed Lineage Kinase Domain-Like (MLKL) bears two clusters of residues that are required for cell death by…”
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Dissecting Specificity in the Janus Kinases: The Structures of JAK-Specific Inhibitors Complexed to the JAK1 and JAK2 Protein Tyrosine Kinase Domains by Williams, Neal K., Bamert, Rebecca S., Patel, Onisha, Wang, Christina, Walden, Patricia M., Wilks, Andrew F., Fantino, Emmanuelle, Rossjohn, Jamie, Lucet, Isabelle S.

“…The Janus kinases (JAKs) are a pivotal family of protein tyrosine kinases (PTKs) that play prominent roles in numerous cytokine signaling pathways, with…”
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The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor by Lucet, Isabelle S., Fantino, Emmanuelle, Styles, Michelle, Bamert, Rebecca, Patel, Onisha, Broughton, Sophie E., Walter, Mark, Burns, Christopher J., Treutlein, Herbert, Wilks, Andrew F., Rossjohn, Jamie

“…JAK2, a member of the Janus kinase (JAK) family of protein tyrosine kinases (PTKs), is an important intracellular mediator of cytokine signaling. Mutations of…”
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Colony-stimulating factor-1 (CSF-1) delivers a proatherogenic signal to human macrophages by Irvine, Katharine M., Andrews, Melanie R., Fernandez‐Rojo, Manuel A., Schroder, Kate, Burns, Christopher J., Su, Stephen, Wilks, Andrew F., Parton, Robert G., Hume, David A., Sweet, Matthew J.

“…M‐CSF/CSF‐1 supports the proliferation and differentiation of monocytes and macrophages. In mice, CSF‐1 also promotes proinflammatory responses in vivo by…”
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Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors by Sharp, Phillip P, Garnier, Jean-Marc, Hatfaludi, Tamas, Xu, Zhen, Segal, David, Jarman, Kate E, Jousset, Hélène, Garnham, Alexandra, Feutrill, John T, Cuzzupe, Anthony, Hall, Peter, Taylor, Scott, Walkley, Carl R, Tyler, Dean, Dawson, Mark A, Czabotar, Peter, Wilks, Andrew F, Glaser, Stefan, Huang, David C. S, Burns, Christopher J

“…A number of diazepines are known to inhibit bromo- and extra-terminal domain (BET) proteins. Their BET inhibitory activity derives from the fusion of an…”
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The Use of JAK-specific inhibitors as chemical biology tools by Burns, Christopher J, Segal, David, Wilks, Andrew F

“…The JAK family of protein tyrosine kinases are now recognized as important participants in a wide range of pathologies, from cancer to inflammatory diseases…”
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The 2.7 Å Crystal Structure of the Autoinhibited Human c-Fms Kinase Domain by Walter, Mark, Lucet, Isabelle S., Patel, Onisha, Broughton, Sophie E., Bamert, Rebecca, Williams, Neal K., Fantino, Emmanuelle, Wilks, Andrew F., Rossjohn, Jamie

“…c-Fms, a member of the Platelet-derived Growth Factor (PDGF) receptor family of receptor tyrosine kinases (RTKs), is the receptor for macrophage colony…”
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CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo by Burns, Christopher J, Fantino, Emmanuelle, Phillips, Ian D, Su, Stephen, Harte, Michael F, Bukczynska, Patricia E, Frazzetto, Mark, Joffe, Max, Kruszelnicki, Irma, Wang, Bing, Wang, Yue, Wilson, Neil, Dilley, Rodney J, Wan, Soo S, Charman, Susan A, Shackleford, David M, Fida, Rosa, Malcontenti-Wilson, Cathy, Wilks, Andrew F

“…CYT997 is a wholly synthetic compound that possesses highly potent cytotoxic activity in vitro through inhibition of microtubule polymerization. CYT997 blocks…”
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The JAK kinases: Not just another kinase drug discovery target by Wilks, Andrew F.

“…There are four members of the JAK family of protein tyrosine kinases (PTKs) in the human genome. Since their discovery in 1989, great strides have been made in…”
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Plasmodium kinases as targets for new-generation antimalarials by Lucet, Isabelle S, Tobin, Andrew, Drewry, David, Wilks, Andrew F, Doerig, Christian

“…There is an urgent need for the development of new antimalarial drugs with novel modes of actions. The malarial parasite, Plasmodium falciparum, has a…”
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c-FMS inhibitors: a patent review by Burns, Christopher J, Wilks, Andrew F

“…Macrophages are key drivers of both the innate and adaptive immune systems. The cellular receptor for CSF-1 and IL-34, c-FMS, is a key component of the…”
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Defining a therapeutic window for kinase inhibitors in leukemia to avoid neutropenia by McArthur, Kate, D'Cruz, Akshay A, Segal, David, Lackovic, Kurt, Wilks, Andrew F, O'Donnell, Joanne A, Nowell, Cameron J, Gerlic, Motti, Huang, David C S, Burns, Christopher J, Croker, Ben A

“…Neutropenia represents one of the major dose-limiting toxicities of many current cancer therapies. To circumvent the off-target effects of cytotoxic…”
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Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs) by Burns, Christopher J., Bourke, David G., Andrau, Laura, Bu, Xianyong, Charman, Susan A., Donohue, Andrew C., Fantino, Emmanuelle, Farrugia, Michelle, Feutrill, John T., Joffe, Max, Kling, Marcel R., Kurek, Margarita, Nero, Tracy L., Nguyen, Thao, Palmer, James T., Phillips, Ian, Shackleford, David M., Sikanyika, Harrison, Styles, Michelle, Su, Stephen, Treutlein, Herbert, Zeng, Jun, Wilks, Andrew F.

“…Details of SAR studies leading to CYT387, a potent and selective dual JAK1 and JAK2 inhibitor, are reported. A series of phenylaminopyrimidines has been…”
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Vascular Endothelial Growth Factor D (VEGF-D) is a Ligand for the Tyrosine Kinases VEGF Receptor 2 (Flk1) and VEGF Receptor 3 (Flt4) by Achen, Marc G., Jeltsch, Michael, Kukk, Eola, Makinen, Taija, Vitali, Angela, Wilks, Andrew F., Alitalo, Kari, Stacker, Steven A.

“…We have identified a member of the VEGF family by computer-based homology searching and have designated it VEGF-D. VEGF-D is most closely related to VEGF-C by…”
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CSF-1 receptor kinase inhibitor targets effector functions and inhibits pro-inflammatory cytokine production from murine macrophage populations by Irvine, Katharine M, Burns, Christopher J, Wilks, Andrew F, Su, Stephen, Hume, David A, Sweet, Matthew J

“…CSF-1 regulates macrophage differentiation, survival, and function, and is an attractive therapeutic target for chronic inflammation and malignant diseases…”
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The microtubule depolymerizing agent CYT997 causes extensive ablation of tumor vasculature in vivo by Burns, Christopher J, Fantino, Emmanuelle, Powell, Andrew K, Shnyder, Steven D, Cooper, Patricia A, Nelson, Stuart, Christophi, Christopher, Malcontenti-Wilson, Cathy, Dubljevic, Valentina, Harte, Michael F, Joffe, Max, Phillips, Ian D, Segal, David, Wilks, Andrew F, Smith, Gregg D

“…The orally active microtubule-disrupting agent (S)-1-ethyl-3-(2-methoxy-4-(5-methyl-4-((1-(pyridin-3-yl)butyl)amino)pyrimidin-2-yl)phenyl)urea (CYT997),…”
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Inhibition of growth of C6 glioma cells in vivo by expression of antisense vascular endothelial growth factor sequence by Saleh, M, Stacker, S A, Wilks, A F

“…Tumor angiogenesis involves a combination of events including the production of inhibitors, proteases, and angiogenic factors that have a chemotactic and…”
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Discovery of CYT997: a structurally novel orally active microtubule targeting agent by Burns, Christopher J., Harte, Michael F., Bu, Xianyong, Fantino, Emmanuelle, Joffe, Max, Sikanyika, Harrison, Su, Stephen, Tranberg, C. Elisabet, Wilson, Neil, Charman, Susan A., Shackleford, David M., Wilks, Andrew F.

“…CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of cancer cells. CYT997 was discovered…”
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Ryk-deficient mice exhibit craniofacial defects associated with perturbed Eph receptor crosstalk by Stacker, Steven A, Halford, Michael M, Armes, Jane, Buchert, Michael, Meskenaite, Virginia, Grail, Dianne, Hibbs, Margaret L, Wilks, Andrew F, Farlie, Peter G, Newgreen, Don F, Hovens, Christopher M

“…Secondary palate formation is a complex process that is frequently disturbed in mammals, resulting in the birth defect cleft palate. Gene targeting has…”
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Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS by Burns, Christopher J., Harte, Michael F., Bu, Xianyong, Fantino, Emmanuelle, Giarrusso, Marilena, Joffe, Max, Kurek, Margarita, Legge, Fiona S., Razzino, Pasquale, Su, Stephen, Treutlein, Herbert, Wan, Soo San, Zeng, Jun, Wilks, Andrew F.

“…A novel series of 2-(α-methylbenzylamino) pyrazines have been synthesized and shown to be potent inhibitors of the FMS tyrosine receptor kinase. A series of…”
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